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Talabostat mesylate

Cat. No. 3719 5 Citations Submit a Review Datasheet / COA / SDS
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Description: Potent DPP IV inhibitor; activates NLRP1b inflammasome
Alternative Names: Val-boroPro, BXCL 701
Chemical Name: B-[(2R)-1-[(2S)-2-Amino-3-methyl-1-oxobutyl]-2-pyrrolidinyl]boronic acid methanesulfonate
Purity: ≥98% (HPLC)
Datasheet
Citations (5)
Reviews
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for Talabostat mesylate

Talabostat mesylate is a potent DPP IV inhibitor (IC50 values are <4, 4, 11, 310 and 560 nM at DPP4, DPP8, DPP9, DPP7 and FAP, respectively). Activates the inflammasome sensor protein NLRP1b and selectively triggers pyroptosis in monocytes and macrophages. Induces immune-mediated tumor regression in multiple mouse models of cancer. Orally bioavailable.

Technical Data for Talabostat mesylate

M. Wt 310.18
Formula C9H19BN2O3.CH3SO3H
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 150080-09-4
PubChem ID 11522448
InChI Key OXYYOEIGQRXGPI-WSZWBAFRSA-N
Smiles O=C([C@@H](N)C(C)C)N1CCC[C@H]1B(O)O.CS(O)(=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Talabostat mesylate

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 31.02 100
DMSO 15.51 50

Preparing Stock Solutions for Talabostat mesylate

The following data is based on the product molecular weight 310.18. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.22 mL 16.12 mL 32.24 mL
5 mM 0.64 mL 3.22 mL 6.45 mL
10 mM 0.32 mL 1.61 mL 3.22 mL
50 mM 0.06 mL 0.32 mL 0.64 mL

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Product Datasheets for Talabostat mesylate

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for Talabostat mesylate

References are publications that support the biological activity of the product.

Okondo et al (2017) DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat.Chem.Biol. 13 46 PMID: 27820798

Okondo et al (2018) Inhibition of Dpp8/9 activates the Nlrp1b inflammasome. Cell Chem.Biol. 25 262 PMID: 29396289

If you know of a relevant reference for Talabostat mesylate, please let us know.

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Keywords: Talabostat mesylate, Talabostat mesylate supplier, Potent, DPP, IV, inhibitors, inhibits, inflammasome, pyroptosis, Nlrp1b, BXCL701, DPP4, Val-boroPro, BXCL, 701, Dipeptidyl, Peptidase, (DPP-IV), Inflammasomes, 3719, Tocris Bioscience

5 Citations for Talabostat mesylate

Citations are publications that use Tocris products. Selected citations for Talabostat mesylate include:

Massimiliano et al (2022) PhAc-ALGP-Dox, a Novel Anticancer Prodrug with Targeted Activation and Improved Therapeutic Index. Mol Cancer Ther 21 568-581 PMID: 35149549

Daniel A et al (2022) A ubiquitin-independent proteasome pathway controls activation of the CARD8 inflammasome. J Biol Chem 298 102032 PMID: 35580636

Justin R et al (2022) M24B aminopeptidase inhibitors selectively activate the CARD8 inflammasome. Nat Chem Biol 18 565-574 PMID: 35165443

Orth-He et al (2023) Protein folding stress potentiates NLRP1 and CARD8 inflammasome activation. Cell Rep 42 111965 PMID: 36649711

Do you know of a great paper that uses Talabostat mesylate from Tocris? Please let us know.

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